Multigram-scale Synthesis of Enantiopure 3,3-Difluoroproline.

ABSTRACT: An efficient route for the synthesis of enantiopure 3,3-difluoroproline on multigram-scale is described herein. The deoxofluorination can be achieved with DAST on the corresponding racemic pyrrolidinone in good yield. Resolution of the racemate by crystallization with D- and L-tyrosine hydrazide provides both enantiomers of 3,3-difluoroproline in high yield and ee%.

SUBMITTER: Doebelin C 

PROVIDER: S-EPMC5456297 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature